2,2-diphenylethyl isothiocyanate

2,2-Diphenylethyl isothiocyanate (DPEITC), also known as SF5, is a synthetic small-molecule research compound and sulforaphane analog. Developed as a more potent synthetic analog of the dietary compound phenethyl isothiocyanate (PEITC) at the Lombardi Comprehensive Cancer Center at Georgetown University, DPEITC is being investigated for its anticancer and renal protective properties. Its primary mechanism of action involves the direct binding, rescue, and reactivation of 'hotspot' mutant p53 proteins (both structural and contact mutants), leading to mutant p53 depletion and the induction of apoptosis in human cancer cells. Additionally, DPEITC suppresses the expression of multi-drug resistance 1 (MDR1) and ETS1, which are associated with chemoresistance, and acts synergistically with topoisomerase inhibitors such as doxorubicin and camptothecin. It has been studied primarily in breast cancer subtypes, including triple-negative, HER2+, and Luminal A, and has shown potential as a renal protective agent in drug-resistant acute renal disease.

Other names

2,2-diphenethyl isothiocyanate2,2-diphenylethyl ITC